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The mechanistic basis of a PAE induced
2022-09-07
The mechanistic basis of a PAE-induced reduction in HDC isoform expression is unclear at present. These reductions may be a consequence of reduced histaminergic innervation of PAE-affected brain regions. Given that these three brain regions are anatomically more distant from the ventral hypothalamus
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A series of P P
2022-09-06
A series of P3-P4 ureas were explored first and their anti-NS3 protease activity, antiviral properties in a HCV replicon cell-based assay and PK profiles examined. Installation of a methyl group on the P4 side nitrogen ras inhibitor of the urea yielded , a molecule which retained intrinsic potency a
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The endocytic inhibitors MDC and CPZ and dynamin GTPase bloc
2022-09-06
The endocytic inhibitors MDC and CPZ and dynamin GTPase blocker (dynamin mutant) have been shown to significantly decrease the intracellular accumulation of cGMP. Moreover, earlier reports suggested that G-protein-coupled receptor (GPCRs) continue to signal by generating cAMP throughout internalizat
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Interestingly studies from Sahai and colleagues in
2022-09-06
Interestingly, studies from Sahai and colleagues in cancer-associated fibroblasts have revealed that YAP is required for the acquirement of a stiff ECM in the tumor microenvironment (Calvo et al., 2013). Subsequently, this stiffening of the matrix can activate YAP, thus creating a feed-forward loop.
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As part of their ongoing effort in the field Kalypsis
2022-09-06
As part of their ongoing effort in the field, Kalypsis recently disclosed that quinazolinones 5 [49], imidazo[1,2-a] [1,2]diazepin 6 [50] and quinolines 7 [51] all had activity as small molecule modulators of TGR5 (Figure 4). Intercept, however, disclosed different bile Oxamic acid derivatives as T
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Next we designed substituents of the position
2022-09-05
Next, we designed substituents of the 6-position. Edge-to-face aromatic interaction between aromatic ring of ligand and Phe162B needed to be retained because the interaction seems to be important for tight binding. 3′-Position of the 6-phenyl group of directs to a hydrophilic space where W1 exists.
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Given and a module N we
2022-09-03
Given and a -module N, we put The right hand side makes sense because we regard g as an Dexlansoprazole of and meanwhile . It is also a skew group ring, identified with via the following equation It follows that becomes a -module, with Analogous to the situation of group representations, the un
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Bacterial GluRS comes in two flavors discriminatory GluRS
2022-09-03
Bacterial GluRS comes in two flavors, discriminatory GluRS (D-GluRS) and non-discriminatory GluRS (ND-GluRS). While D-GluRS exclusively catalyses the transfer of Glu to tRNAGlu, the ND-GluRS can also glutamylate tRNAGln forming Glu-tRNAGln. The misacylated product is then transformed to Gln-tRNAGln
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br Acknowledgments br Introduction Postmenopausal osteoporos
2022-09-03
Acknowledgments Introduction Postmenopausal osteoporosis, which is primarily caused by 1,4-DPCA deficiency, has been a worldwide health problem and threatens postmenopausal women of all races. An estimated 80% of osteoporosis patients in the United States are women, and approximately 30% of po
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The present study showed that the FPR
2022-09-03
The present study showed that the FPR2 antagonists PBP10 and BOC2 are potent antiviral molecules in vitro against a broad range of IAV and B viruses. Consistently, our previous report showed that FPR2 plays a deleterious role during IAV infections and that another FPR2 antagonist WRW4 inhibits IAV
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Receptor interactions and binding mode of
2022-09-03
Receptor interactions and binding mode of in hGPR40 were determined by docking studies. The compound was docked in the rebuilt co-crystal structure of hGPR40 (PDB ID: ) using MOE for loop modeling and energy minimization and Glide for molecular docking. The docking site used for the docking simulat
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Saxagliptin Our results further indicate that low expression
2022-09-03
Our results further indicate that low expression of p300/CBP in CRC is directly associated with poor clinical therapeutic outcome of 5-FU treatment, potentially providing a new set of biomarkers to predict chemo-sensitivity. Although the ability of low expression of p300/CBP to predict poor prognosi
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br Experimental procedures br Results Hdc KO mice
2022-09-03
Experimental procedures Results Hdc-KO mice show basal activation of the MAPK and AKT/GSK3β pathways in the dorsal striatum (Rapanelli et al., 2014). These signaling pathways are differentially regulated by the H3 receptor in dMSNs and iMSNs in wild-type mice (Rapanelli et al., 2016). To bette
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Migration chemotaxis and trafficking of leukocytes including
2022-09-03
Migration, chemotaxis and trafficking of leukocytes, including eosinophils from the peripheral blood into the site of inflammation requires their adhesion to endothelial Hordenine (Ley et al., 2007). Despite ongoing research, the histamine effect on eosinophils adhesion to endothelium cells has not
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MAP Ks act at the level of MST to
2022-09-03
MAP4Ks act at the level of MST1/2 to phosphorylate LATS1/2 and regulate the Hippo pathway (Box 1). Of particular interest is the involvement of MAP4K4, a key metabolic regulator [88] and common polymorphisms in the MAP4K4 locus are associated with T2D and insulin resistance [89] in adipogenesis. In
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